KDM-IN-1
KDM-IN-1 is a potent Jumonji C domain-containing KDM inhibitor with IC50 values of 1.59, 4.67, 4.76, 1.56, and 1.25 μM against KDM6B, KDM6A, KDM3B, KDM4A, and KDM5B, respectively. KDM-IN-1 acts as a non-competitive inhibitor that inhibits histone demethylation by introducing steric hindrance near the catalytic core (specifically upregulating H3K27me3 levels), thereby inducing DNA damage, cell cycle arrest, and apoptosis. KDM-IN-1 can be used for research on cervical cancer.
For research use only. We do not sell to patients.
- Formula: C21H20N6O3
- Molecular Weight:404.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
KDM6B 1.59 μM (IC50) |
KDM6A 4.67 μM (IC50) |
KDM3B 4.76 μM (IC50) |
KDM4A 1.56 μM (IC50) |
KDM5B 1.25 μM (IC50) |
Caspase-3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| C-33-A | IC50 |
0.813 μM
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Cytotoxicity against human C33A cervical cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
Cytotoxicity against human C33A cervical cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
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42911740 |
| HeLa | IC50 |
3.730 μM
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Cytotoxicity against human HeLa cervical cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
Cytotoxicity against human HeLa cervical cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
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42911740 |
| FaDu | IC50 |
1.858 μM
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Cytotoxicity against human FaDu cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
Cytotoxicity against human FaDu cancer cells assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
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42911740 |
| HaCaT | IC50 |
4.174 μM
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Cytotoxicity against human HaCaT keratinocytes assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
Cytotoxicity against human HaCaT keratinocytes assessed as viability reduction after 24 hrs exposure by CCK-8 assay.
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42911740 |
In Vitro
KDM-IN-1 (0.1-10 μM; 10-14 days of recovery after 24 h administration) inhibits colony formation in the C33A cell line, with complete inhibition at 1 μM[1].
KDM-IN-1 (0.1-1 μM; 24 h) dose-dependently upregulates H3K27me3 and H3K27me2 protein expression levels in the C33A cell line and the HeLa cell line, without affecting H3K4me3 and H3K9me3 protein expression levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C33A cells
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Concentration:1, 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis in a concentration-dependent manner.
At 1 μM, only a modest increase in apoptosis was observed, whereas a pronounced apoptotic response was triggered at 10 μM.
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Cell Line:C33A cells
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Concentration:0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Significantly disrupted cell-cycle progression.
Compared to the control group, it decreased the fraction of cells in G1 and S phases and caused a concomitant accumulation (arrest) of cells in the G2 phase (particularly evident at 2 μM).
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Cell Line:C33A and HeLa cells
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Concentration:0.1, 0.5, 1 μM
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Incubation Time:24 h
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Result:Significantly and concentration-dependently upregulated the intracellular protein levels of H3K27me3 (especially at 0.5 and 1 μM), accompanied by a modest increase in H3K27me2; whereas total H3, H3K27me1, and H3K27ac levels showed no consistent or significant changes.
Did not alter the protein expression levels of H3K4me3 and H3K9me3, demonstrating substrate preference in its regulation of epigenetic modifications.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCG (NOD/ShiLtJGpt-Prkdc^em26Cd52 Il2rg^em26Cd22/Gpt; female; 6-8 weeks old)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.p.; once daily; D14-35, total 21 days
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Result:Significantly inhibited the volume growth of xenograft tumors in a dose-dependent manner, with the 50 mg/kg dose showing superior inhibition over the 25 mg/kg dose.
Significantly and dose-dependently decreased the expression of the proliferation marker Ki-67 in tumor tissues, while drastically increasing the expression levels of the apoptosis executioner Cleaved caspase-3 and the DNA double-strand break marker p-Histone H2A.X (Ser139).
Effectively engaged its epigenetic target in vivo, triggering a significant, dose-dependent upregulation and accumulation of the H3K27me3 modification level in the tumor tissues.
Chemical Information
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Molecular Weight 404.42
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Formula C21H20N6O3
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SMILES
N=C1NCCCN1C2=NC(C3=CC=CC([N+]([O-])=O)=C3)=CC(C4=CC=C(OC)C=C4)=N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KDM-IN-1 Related Classifications
HY-190877 Related Classifications
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